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Dapivirine

Cat. No. M2575
Dapivirine Structure
Synonym:

TMC120; R147681

Size Price Availability Quantity
5mg USD 88  USD88 In stock
10mg USD 125  USD125 In stock
25mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

Dapivirine is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, including a wide range of NNRTI-resistant isolates.

Chemical Information
Molecular Weight 329.4
Formula C20H19N5
CAS Number 244767-67-7
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Neeraja Bhavaraju, et al. Introducing the Dapivirine Vaginal Ring in Sub-Saharan Africa: What Can We Learn from Oral PrEP?

[2] Anita Kabarambi, et al. The dapivirine vaginal ring from the perspective of married men in Uganda

[3] Elizabeth R Brown, et al. Greater dapivirine release from the dapivirine vaginal ring is correlated with lower risk of HIV-1 acquisition: a secondary analysis from a randomized, placebo-controlled trial

[4] Christina Farr Zuend, et al. Influence of dapivirine vaginal ring use on cervicovaginal immunity and functional microbiome in adolescent girls

[5] Krishnaveni Reddy, et al. Use of the dapivirine vaginal ring and effect on cervical cytology abnormalities

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Keywords: Dapivirine, TMC120; R147681 supplier, Reverse Transcriptase, inhibitors, activators


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